UPNEEQ
Clinical safety rating: caution
Comprehensive clinical and safety monograph for UPNEEQ (UPNEEQ).
Oxymetazoline is an alpha-1A adrenoceptor agonist, causing vasoconstriction of the ophthalmic artery to reduce eyelid edema.
| Metabolism | Not significantly metabolized; primarily excreted unchanged in urine. |
| Excretion | Primarily renal elimination of unchanged drug (approximately 60-70% of the dose excreted unchanged in urine) with biliary/fecal elimination accounting for the remainder (~30-40% as metabolites and unchanged drug). |
| Half-life | Terminal elimination half-life of 1.5-2 hours in healthy adults; may be prolonged in severe hepatic impairment due to reduced metabolism. |
| Protein binding | Approximately 30-40% bound to plasma proteins (albumin). |
| Volume of Distribution | Volume of distribution is approximately 1.5-2.0 L/kg, indicating distribution beyond plasma into interstitial fluid and tissues. |
| Bioavailability | Systemic bioavailability after topical ocular administration is low (<5% of administered dose reaches systemic circulation); negligible oral bioavailability due to extensive first-pass metabolism. |
| Onset of Action | When applied topically to the eyelid, onset of action occurs within 1-5 minutes, with maximal effect achieved within 15-30 minutes. |
| Duration of Action | Duration of effect on upper eyelid retraction and eyelid elevation lasts approximately 6-8 hours after a single dose, sufficient for daily use in cosmetic or therapeutic settings. |
| Molecular Weight | 296.4 |
1 drop in each eye once daily in the evening.
| Dosage form | SOLUTION/DROPS |
| Renal impairment | No dose adjustment required for renal impairment. |
| Liver impairment | No dose adjustment required for hepatic impairment. |
| Pediatric use | Safety and efficacy not established in pediatric patients. |
| Geriatric use | No specific dose adjustment recommended; use standard adult dosing. |
| 1st trimester | No adequate studies in pregnant women. Use only if potential benefit justifies risk. |
| 2nd trimester | No adequate studies in pregnant women. Use only if potential benefit justifies risk. |
| 3rd trimester | No adequate studies in pregnant women. Use only if potential benefit justifies risk. |
Clinical note
Comprehensive clinical and safety monograph for UPNEEQ (UPNEEQ).
| Placental transfer | Unknown; no data available on placental transfer. |
| Breastfeeding | Not known if oxymetazoline is excreted in human milk. Caution advised due to potential for cardiovascular effects in infant. |
| Lactation Rating |
■ FDA Black Box Warning
None
| Serious Effects |
Hypersensitivity to oxymetazoline or any componentAngle-closure glaucomaRhinitis sicca
| Precautions | May cause anisocoria (unequal pupil size) due to mydriasis, Avoid use in patients with narrow-angle glaucoma, Use with caution in patients with cardiovascular disease (e.g., hypertension, arrhythmias) or hyperthyroidism, May cause burning/stinging or blurred vision upon instillation, Not recommended for children under 6 years of age |
| Food/Dietary | No known food interactions. Avoid alcohol and caffeine as they may worsen side effects like insomnia or nervousness. |
| Clinical Pearls |
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| L3 |
| Teratogenic Risk | Upneeq (oxymetazoline) is an alpha-1 agonist intended for topical ophthalmic use. Systemic absorption is minimal, but based on drug class, first trimester vascular disruption cannot be ruled out. Animal studies with high IV doses showed teratogenicity, but no adequate human data. Risk in first trimester: potential vascular effects; second/third trimester: possible uterine contractions if systemic absorption occurs, though unlikely with ocular dosing. Overall, risk is low due to minimal systemic exposure. |
| Fetal Monitoring | Maternal: Monitor for hypertension, tachycardia, or local ocular effects. Fetal: No specific monitoring required because of minimal systemic exposure. However, if high doses or prolonged use occur, monitor fetal growth and uterine activity via ultrasound and fetal heart rate monitoring. |
| Fertility Effects | No known adverse effects on fertility based on limited data. Animal studies with high systemic doses showed no impairment of fertility. Ophthalmic use is unlikely to affect reproduction. |
| Upneeq (oxymetazoline ophthalmic) is an alpha-1 adrenergic receptor agonist indicated for acquired blepharoptosis. It causes contraction of the Müller muscle to elevate the upper eyelid. Do not use in patients with narrow-angle glaucoma or uncontrolled hypertension. Onset within 15 minutes, duration up to 6 hours. Apply one drop per eye once daily. Avoid touching dropper tip to any surface. |
| Patient Advice | Use exactly as directed: one drop in each eye once daily. · Do not touch the dropper tip to your eye or any surface to avoid contamination. · Remove contact lenses before use and wait at least 15 minutes before reinserting. · May cause temporary blurred vision; do not drive or operate machinery until vision clears. · Report any eye pain, vision changes, or worsening redness to your doctor. · Do not use more than once daily; overuse can cause adverse effects. |